EP3307067A4 - Aminopyrazine compounds with a2a antagonist properties - Google Patents
Aminopyrazine compounds with a2a antagonist properties Download PDFInfo
- Publication number
- EP3307067A4 EP3307067A4 EP16808075.2A EP16808075A EP3307067A4 EP 3307067 A4 EP3307067 A4 EP 3307067A4 EP 16808075 A EP16808075 A EP 16808075A EP 3307067 A4 EP3307067 A4 EP 3307067A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- antagonist properties
- aminopyrazine compounds
- aminopyrazine
- compounds
- antagonist
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
- A01N43/80—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Plant Pathology (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Neurology (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Environmental Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Dispersion Chemistry (AREA)
- Toxicology (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562174295P | 2015-06-11 | 2015-06-11 | |
| PCT/US2016/035960 WO2016200717A1 (en) | 2015-06-11 | 2016-06-06 | Aminopyrazine compounds with a2a antagonist properties |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EP3307067A1 EP3307067A1 (en) | 2018-04-18 |
| EP3307067A4 true EP3307067A4 (en) | 2018-12-05 |
| EP3307067B1 EP3307067B1 (en) | 2022-11-02 |
Family
ID=57503919
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP16808075.2A Active EP3307067B1 (en) | 2015-06-11 | 2016-06-06 | Aminopyrazine compounds with a2a antagonist properties |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US10688082B2 (en) |
| EP (1) | EP3307067B1 (en) |
| WO (1) | WO2016200717A1 (en) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12414952B2 (en) | 2018-11-20 | 2025-09-16 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| AU2019383948A1 (en) | 2018-11-20 | 2021-05-20 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| WO2020112700A1 (en) | 2018-11-30 | 2020-06-04 | Merck Sharp & Dohme Corp. | 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| AU2019388872A1 (en) | 2018-11-30 | 2021-05-27 | Merck Sharp & Dohme Llc | 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| MX2021008094A (en) | 2019-01-11 | 2021-09-21 | Omeros Corp | METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCER. |
| WO2022020550A1 (en) * | 2020-07-24 | 2022-01-27 | Merck Sharp & Dohme Corp. | Adenosine a2a and a2b receptor dual antagonists for immuno-oncology |
| JP2025512384A (en) | 2022-04-13 | 2025-04-17 | ギリアード サイエンシーズ, インコーポレイテッド | Combination Therapies for Treating TROP-2-Expressing Cancers |
| US12516018B2 (en) * | 2023-03-30 | 2026-01-06 | Brandeis University | Solid-solid phase change aromatic azo compounds, method of manufacture, and use for thermal energy storage and release |
| WO2025137640A1 (en) | 2023-12-22 | 2025-06-26 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
| US12180208B1 (en) * | 2024-01-19 | 2024-12-31 | King Faisal University | Pyrazolo[1,5-c]pyrido[3,4-e]pyrimidines as CK2 inhibitors |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3531482A (en) * | 1966-10-13 | 1970-09-29 | Sandoz Ag | Pyrazolo(1,5-c)quinazolines |
| IT1264901B1 (en) | 1993-06-29 | 1996-10-17 | Schering Plough S P A | HETEROCYCLIC ANALOGUES OF 1,2,4-TRIAZOLE(15-C)PYRIMIDINES WITH ANTAGONIST ACTIVITY FOR THE ADENOSINE A2 RECEPTOR |
| WO1995003806A1 (en) | 1993-07-27 | 1995-02-09 | Kyowa Hakko Kogyo Co., Ltd. | Remedy for parkinson's disease |
| IT1277392B1 (en) | 1995-07-28 | 1997-11-10 | Schering Plough S P A | HEROCYCLIC ANALOGS OF 1,2,4-TRIAZOLE (1,5-C] PYRIMIDINE WITH ANTAGONIST ACTIVITY FOR THE A2A RECEPTOR OF ADENOSINE |
| IT1291372B1 (en) | 1997-05-21 | 1999-01-07 | Schering Plough S P A | USE OF HETEROCYCLIC ANALOGS OF 1,2,4-TRIAZOLE (1,5-C) PYRIMIDINS FOR THE PREPARATION OF MEDICATIONS USEFUL FOR THE TREATMENT OF DISEASES |
| DE60110219T2 (en) | 2000-05-26 | 2006-03-09 | Schering Corp. | ADENOSINE A2A RECEPTOR ANTAGONISTS |
| AR073574A1 (en) * | 2008-09-10 | 2010-11-17 | Alcon Res Ltd | HETEROCICLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF A DISEASE |
| US20150174130A1 (en) * | 2012-07-26 | 2015-06-25 | Vanderbilt University | Compositions and methods for treating microbial infections |
| WO2014101120A1 (en) * | 2012-12-28 | 2014-07-03 | Merck Sharp & Dohme Corp. | Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
| WO2015027431A1 (en) * | 2013-08-29 | 2015-03-05 | Merck Sharp & Dohme Corp. | 2,2-difluorodioxolo a2a receptor antagonists |
-
2016
- 2016-06-06 WO PCT/US2016/035960 patent/WO2016200717A1/en not_active Ceased
- 2016-06-06 US US15/815,212 patent/US10688082B2/en active Active
- 2016-06-06 EP EP16808075.2A patent/EP3307067B1/en active Active
Non-Patent Citations (3)
| Title |
|---|
| CATARZI D ET AL: "Pyrazolo[1,5-c]quinazoline derivatives and their simplified analogues as adenosine receptor antagonists: Synthesis, structure-affinity relationships and molecular modeling studies", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 21, no. 1, 1 January 2013 (2013-01-01), pages 283 - 294, XP028961394, ISSN: 0968-0896, DOI: 10.1016/J.BMC.2012.10.031 * |
| See also references of WO2016200717A1 * |
| YANG X ET AL: "Easy and efficient one-pot synthesis of pyrazolo[1,5-c]quinazolines under mild copper-catalyzed conditions", RSC ADVANCES, vol. 2, no. 29, 19 September 2012 (2012-09-19), pages 11061, XP055516027, ISSN: 2046-2069, DOI: 10.1039/c2ra21929h * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3307067A1 (en) | 2018-04-18 |
| US20180193314A1 (en) | 2018-07-12 |
| EP3307067B1 (en) | 2022-11-02 |
| WO2016200717A1 (en) | 2016-12-15 |
| US10688082B2 (en) | 2020-06-23 |
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